Cancer is the predominant and major cause of fatality worldwide, based on the different types of cancer. There is a limitation in the current treatment. So we need better therapeutic agents that counteract the progression and development of malignant tumours. Plant-derived products are closely related and useful for human health. Luteolin is a polyphenolic flavonoid bioactive molecule that is present in various herbs, vegetables, fruits, and flowers and exhibits chemoprotective and pharmacological activity against different malignancies. To offer innovative approaches for the management of various cancers, we present a comprehensive analysis of the latest discoveries on luteolin. The aim is to inspire novel concepts for the development of advanced pharmaceuticals targeting cancer and search specifically targeted reviews and research articles published from January 1999 to January 2024 that investigated the application of luteolin in various cancer management. A thorough literature search utilizing the keywords "luteolin" "Signalling Pathway" "cancer" and nanoparticles was performed in the databases of Google Scholar, Web of Science, SCOPUS, UGC care list and PubMed. Through the compilation of existing research, we have discovered that luteolin possesses several therapeutic actions against various cancer via a signaling pathway involving the of NF-κB regulation, AMPK/mTOR, toll-like receptor, Nrf-2, PI3K/Akt MAPK and Wnt/β-catenin and their underlying mechanism of action has been well understood. This review intended to completely integrate crucial information on natural sources, biosynthesis, pharmacokinetics, signaling pathways, chemoprotective and therapeutic properties against various cancers, and nanoformulation of luteolin.